Interaction of phytoestrogens with estrogen receptors alpha and beta (II).

Keiko Morito, Tohru Aomori, Toshiharu Hirose, Junei Kinjo, Junichi Hasegawa, Sumito Ogawa, Satoshi Inoue, Masami Muramatsu, Yukito Masamune

Research output: Contribution to journalArticlepeer-review

141 Citations (Scopus)


We investigated the estrogenic activities of isoflavone derivatives in competition binding assays with human estrogen receptor (hER) alpha or hER beta protein, and in a gene expression assay using a yeast system. Coumestrol binds as strongly as 17beta-estradiol to both hERs. Biochanin A, 5-OMe-genistein, formononetin, and tectorigenin bind well to hER beta, but significant binding to hER alpha is only observed with 5-OMe-genistein, formononetin and tectorigenin. The binding of 7-OMe-genistein and irisolidone is poor to both receptors. Among the glucosides, sissotorin binds both receptors and the binding is stronger than genistin. Coumestrol induces transcription as strongly as genistein. Tectorigenin also induces transcription with both hERs. Though biochanin A, 5-OMe-genistein, 7-OMe-genistein, irisolidone and formononetin slightly induce transcription with hER beta, they act as antagonists in the induction of transcription by 17beta-estradiol. The results show that methylation or glucosidation of isoflavones generally inhibits their phytoestrogenic activities.

Original languageEnglish
Pages (from-to)48-52
Number of pages5
JournalBiological & pharmaceutical bulletin
Issue number1
Publication statusPublished - 2002 Jan
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science


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